Claims (15)
1. Spoj s formulom (IV)
gdje
Het1 je pirazolil, koji može biti nesupstituiran ili mono-, di- ili trisupstituiran, neovisno jedan od drugoga sa Hal ili A,
A u svakom slučaju neovisno označava nerazgranati ili razgranati alkil koji ima 1, 2, 3, 4, 5 ili 6 C atoma, gdje, međusobno neovisno, 1, 2, 3, 4, ili 5 H atoma mogu biti zamijenjeni s Hal,
Hal predstavlja F, Cl, Br ili I,
HET je odabran od: 3-difluorometoksi-5-fluoropiridin-4-il, 3-fluoro-5-metoksipiridin-4-il, 3-fluoro-5-fluorometoksipiridin-4-il, 3-fluoro-5-(trideuteriometoksi)piridin-4-il,
i/ili njihovog farmaceutski upotrebljivog derivata, soli, solvata, tautomera, stereoizomera.1. Compound with formula (IV)
where
Het1 is pyrazolyl, which can be unsubstituted or mono-, di- or trisubstituted, independently of each other with Hal or A,
A in each case independently denotes straight or branched alkyl having 1, 2, 3, 4, 5 or 6 C atoms, where, independently of each other, 1, 2, 3, 4, or 5 H atoms may be replaced by Hal,
Hal represents F, Cl, Br or I,
HET is selected from: 3-difluoromethoxy-5-fluoropyridin-4-yl, 3-fluoro-5-methoxypyridin-4-yl, 3-fluoro-5-fluoromethoxypyridin-4-yl, 3-fluoro-5-(trideuteriomethoxy) pyridin-4-yl,
and/or their pharmaceutically usable derivatives, salts, solvates, tautomers, stereoisomers.
2. Spoj s formulom (IV) prema zahtjevu 1, naznačen time što je Het1 odabran iz niza koji sadrži: 1H-pirazol-4-il, 2H-pirazol-3-il, 1H-pirazol-3-il, 1-metil-1H-pirazol-4-il, 3-metil-1H-pirazol-4-il, 5-metil-1H-pirazol-3-il, 4-metil-1H-pirazol-3-il, 1-fluorometil-1H-pirazol-4-il, 1-difluorometil-1H-pirazol-4-il, 1,3-dimetil-1H-pirazol-4-il, 1-etil-1H-pirazol-4-il, 1-etil-3-metil-1H-pirazolil, 3-fluoro-1-metil-1H-pirazol-4-il,
i/ili njihov farmaceutski upotrebljiv derivat, sol, solvat, tautomer, stereoizomer.2. Compound with formula (IV) according to claim 1, characterized in that Het1 is selected from the group containing: 1H-pyrazol-4-yl, 2H-pyrazol-3-yl, 1H-pyrazol-3-yl, 1-methyl -1H-pyrazol-4-yl, 3-methyl-1H-pyrazol-4-yl, 5-methyl-1H-pyrazol-3-yl, 4-methyl-1H-pyrazol-3-yl, 1-fluoromethyl-1H -pyrazol-4-yl, 1-difluoromethyl-1H-pyrazol-4-yl, 1,3-dimethyl-1H-pyrazol-4-yl, 1-ethyl-1H-pyrazol-4-yl, 1-ethyl-3 -methyl-1H-pyrazolyl, 3-fluoro-1-methyl-1H-pyrazol-4-yl,
and/or their pharmaceutically usable derivative, salt, solvate, tautomer, stereoisomer.
3. Spoj prema zahtjevu 1, naznačen time što je odabran od3. A compound according to claim 1, characterized in that it is selected from
i/ili njegov farmaceutski upotrebljiv derivat, sol, solvat, tautomer, stereoizomer.and/or its pharmaceutically usable derivative, salt, solvate, tautomer, stereoisomer.
4. Spoj prema jednom od zahtjeva 1 do 3 i/ili njegov farmaceutski upotrebljiv derivat, sol, solvat, tautomer ili stereoizomer, naznačen time što je za uporabu kao lijek.4. A compound according to one of claims 1 to 3 and/or its pharmaceutically usable derivative, salt, solvate, tautomer or stereoisomer, characterized in that it is for use as a medicine.
5. Spoj prema jednom od zahtjeva 1 do 3 i/ili njegov farmaceutski upotrebljiv derivat, sol, solvat, tautomer ili stereoizomer, naznačen time što je za uporabu u liječenju raka, tumora i/ili metastaza.5. A compound according to one of claims 1 to 3 and/or its pharmaceutically usable derivative, salt, solvate, tautomer or stereoisomer, characterized in that it is for use in the treatment of cancer, tumors and/or metastases.
6. Spoj prema jednom od zahtjeva 1 do 3 i/ili njegov farmaceutski upotrebljiv derivat, sol, solvat, tautomer, stereoizomer, naznačen time što je za uporabu u liječenju raka, tumora i/ili metastaza u kombinaciji s radioterapijom.6. A compound according to one of claims 1 to 3 and/or its pharmaceutically usable derivative, salt, solvate, tautomer, stereoisomer, characterized in that it is for use in the treatment of cancer, tumors and/or metastases in combination with radiotherapy.
7. Spoj prema jednom od zahtjeva 1 do 3 i/ili njegov farmaceutski upotrebljiv derivat, sol, solvat, tautomer, stereoizomer naznačen time što je za uporabu u liječenju raka, tumora i/ili metastaza u kombinaciji s najmanje jednim antikancerogenim sredstvom.7. A compound according to one of claims 1 to 3 and/or its pharmaceutically usable derivative, salt, solvate, tautomer, stereoisomer, characterized in that it is for use in the treatment of cancer, tumors and/or metastases in combination with at least one anticancer agent.
8. Spoj i/ili njegov farmaceutski upotrebljiv derivat, sol, solvat, tautomer, stereoizomer za uporabu prema jednom od patentnih zahtjeva 5 do 7 naznačen time što je tumor odabran iz skupine bolesti skvamoznog epitela, mjehura, želuca, bubrega, glave, vrata, jednjaka, grlića maternice, štitnjače, crijeva, kosti, jetre, mozga, prostate, urogenitalnog trakta, limfnog sustava, grkljana, pluća, kože, krvi i imunološkog sustava, i/ili rak je odabran iz skupine koju čine monocitna leukemija, adenokarcinom pluća, karcinom pluća malih stanica, rak gušterače, glioblastom, karcinom crijeva, karcinom dojke, akutna mijeloična leukemija, kronična mijeloična leukemija, akutna limfatična leukemija, kronična limfatična leukemija, Hodgkinov limfom i ne-Hodgkinov limfom.8. Compound and/or its pharmaceutically usable derivative, salt, solvate, tautomer, stereoisomer for use according to one of patent claims 5 to 7 characterized in that the tumor is selected from the group of diseases of squamous epithelium, bladder, stomach, kidney, head, neck, esophagus, cervix, thyroid, intestine, bone, liver, brain, prostate, urogenital tract, lymphatic system, larynx, lung, skin, blood and immune system, and/or the cancer is selected from the group consisting of monocytic leukemia, lung adenocarcinoma, small cell lung cancer, pancreatic cancer, glioblastoma, bowel cancer, breast cancer, acute myeloid leukemia, chronic myeloid leukemia, acute lymphatic leukemia, chronic lymphatic leukemia, Hodgkin's lymphoma and non-Hodgkin's lymphoma.
9. Farmaceutski pripravak naznačen time što sadrži učinkovitu količinu najmanje jednog spoja prema jednom od zahtjeva 1 do 3 i/ili njegov farmaceutski upotrebljiv derivat, sol, solvat, tautomer ili stereoizomer, po izboru zajedno s najmanje jednom farmaceutski podnošljivom pomoćnom tvari.9. Pharmaceutical preparation characterized in that it contains an effective amount of at least one compound according to one of claims 1 to 3 and/or its pharmaceutically usable derivative, salt, solvate, tautomer or stereoisomer, optionally together with at least one pharmaceutically acceptable excipient.
10. Farmaceutski pripravak prema zahtjevu 9, naznačen time što nadalje sadrži najmanje jedno antikancerogeno sredstvo.10. Pharmaceutical preparation according to claim 9, characterized in that it further contains at least one anticancer agent.
11. Komplet naznačen time što sadrži zasebna pakiranja
(a) učinkovite količine spoja prema jednom od zahtjeva 1 do 3 i/ili njegov farmaceutski upotrebljiv derivat, sol, solvat, tautomer ili stereoizomer, i
(b) učinkovite količine daljnjeg antikancernog sredstva.11. A set characterized by the fact that it contains separate packages
(a) effective amounts of a compound according to one of claims 1 to 3 and/or a pharmaceutically usable derivative, salt, solvate, tautomer or stereoisomer thereof, and
(b) an effective amount of a further anticancer agent.
12. Farmaceutski pripravak prema zahtjevu 10, naznačen time što je najmanje jedno antikancerogeno sredstvo odabrano od sredstava za alkiliranje, spojeva platine, inhibitora topoizomeraze, inhibitora poli-(ADP-riboza)-polimeraze (PARP), inhibitora ATR (ataksija telangiektazija i Rad3 povezanih), antikancerogenih antibiotika i alfa emitera.12. Pharmaceutical preparation according to claim 10, characterized in that at least one anticancer agent is selected from alkylating agents, platinum compounds, topoisomerase inhibitors, poly-(ADP-ribose)-polymerase (PARP) inhibitors, ATR inhibitors (ataxia telangiectasia and Rad3-related ), anticancer antibiotics and alpha emitters.
13. Farmaceutski pripravak prema zahtjevu 10, naznačen time što je najmanje jedno antikancerogeno sredstvo odabrano iz skupa koji sadrži altretamin, bendamustin, busulfan, karmustin, klorambucil, klormetin, ciklofosfamid, dakarbazin, ifosfamid, improsulfan tozilat, lomustin, melfalan, mitobronitol, mitolaktol, nimustin, ranimustin, temozolomid, tiotepa, treosulfan, mekloretamin, karbokvon, apazikuon, fotemustin, glufosfamid, palifosfamid, pipobroman, trofosfamid, uramustin; karboplatin, cisplatin, eptaplatin, miriplatin hidrat, oksaliplatin, lobaplatin, nedaplatin, pikoplatin, satraplatin; etopozid, irinotekan, razoksan, sobuzoksan, topotekan, kamptotecin, doksorubicin, amsakrin; talazoparib, olaparib, veliparib, rukaparib, CEP 9722, MK4827, BGB-290; VE-822, AZ20, AZD6738; amrubicin, bisantren, decitabin, mitoksantron, prokarbazin, trabektedin, klofarabin, amsakrin, brostalicin, piksantron, laromustin; bleomicin, daktinomicin, doksorubicin, epirubicin, idarubicin, levamizol, miltefozin, mitomicin C, romidepsin, streptozocin, valrubicin, zinostatin, zorubicin, daunurobicin, plikamicin, aklarubicin, peplomicin, pirarubicin.13. Pharmaceutical preparation according to claim 10, characterized in that at least one anticancer agent is selected from the group containing altretamine, bendamustine, busulfan, carmustine, chlorambucil, chlormethine, cyclophosphamide, dacarbazine, ifosfamide, improsulfan tosylate, lomustine, melphalan, mitobronitol, mitolactol, nimustine, ranimustine, temozolomide, thiotepa, treosulfan, mechlorethamine, carboquone, apaziquone, fotemustine, glufosfamide, palifosfamide, pipobroman, trofosfamide, uramustine; carboplatin, cisplatin, heptaplatin, miriplatin hydrate, oxaliplatin, lobaplatin, nedaplatin, picoplatin, satraplatin; etoposide, irinotecan, razoxane, sobuzoxan, topotecan, camptothecin, doxorubicin, amsacrine; talazoparib, olaparib, veliparib, rucaparib, CEP 9722, MK4827, BGB-290; VE-822, AZ20, AZD6738; amrubicin, bisantrene, decitabine, mitoxantrone, procarbazine, trabectedin, clofarabine, amsacrine, brostalicin, pixantrone, laromustine; bleomycin, dactinomycin, doxorubicin, epirubicin, idarubicin, levamisole, miltefosine, mitomycin C, romidepsin, streptozocin, valrubicin, zinostatin, zorubicin, daunurobicin, plicamycin, aclarubicin, peplomycin, pirarubicin.
14. Komplet prema zahtjevu 11, naznačen time što je daljnje antikancerogeno sredstvo odabrano od sredstava za alkiliranje, spojeva platine, inhibitora topoizomeraze, inhibitora poli-(ADP-riboza)-polimeraze (PARP), inhibitora ATR (ataksija telangiektazija i Rad3 povezanih), antikancerogenih antibiotika i alfa emitera.14. Kit according to claim 11, characterized in that the further anticancer agent is selected from alkylating agents, platinum compounds, topoisomerase inhibitors, poly-(ADP-ribose)-polymerase (PARP) inhibitors, ATR (ataxia telangiectasia and Rad3-related) inhibitors, anticancer antibiotics and alpha emitters.
15. Komplet prema zahtjevu 11, naznačen time što je najmanje jedno antikancerogeno sredstvo odabrano iz skupa koji sadrži altretamin, bendamustin, busulfan, karmustin, klorambucil, klormetin, ciklofosfamid, dakarbazin, ifosfamid, improsulfan tozilat, lomustin, melfalan, mitobronitol, mitolaktol, nimustin, ranimustin, temozolomid, tiotepa, treosulfan, mekloretamin, karbokvon, apazikuon, fotemustin, glufosfamid, palifosfamid, pipobroman, trofosfamid, uramustin; karboplatin, cisplatin, eptaplatin, miriplatin hidrat, oksaliplatin, lobaplatin, nedaplatin, pikoplatin, satraplatin; etopozid, irinotekan, razoksan, sobuzoksan, topotekan, kamptotecin, doksorubicin, amsakrin; talazoparib, olaparib, veliparib, rukaparib, CEP 9722, MK4827, BGB-290; VE-822, AZ20, AZD6738; amrubicin, bisantren, decitabin, mitoksantron, prokarbazin, trabektedin, klofarabin, amsakrin, brostalicin, piksantron, laromustin; bleomicin, daktinomicin, doksorubicin, epirubicin, idarubicin, levamizol, miltefozin, mitomicin C, romidepsin, streptozocin, valrubicin, zinostatin, zorubicin, daunurobicin, plikamicin, aklarubicin, peplomicin, pirarubicin.15. Kit according to claim 11, characterized in that at least one anticancer agent is selected from the group containing altretamine, bendamustine, busulfan, carmustine, chlorambucil, chlormethine, cyclophosphamide, dacarbazine, ifosfamide, improsulfan tosylate, lomustine, melphalan, mitobronitol, mitolactol, nimustine , ranimustine, temozolomide, thiotepa, treosulfan, mechlorethamine, carboquone, apaziquone, fotemustine, glufosfamide, palifosfamide, pipobroman, trofosfamide, uramustine; carboplatin, cisplatin, heptaplatin, miriplatin hydrate, oxaliplatin, lobaplatin, nedaplatin, picoplatin, satraplatin; etoposide, irinotecan, razoxane, sobuzoxan, topotecan, camptothecin, doxorubicin, amsacrine; talazoparib, olaparib, veliparib, rucaparib, CEP 9722, MK4827, BGB-290; VE-822, AZ20, AZD6738; amrubicin, bisantrene, decitabine, mitoxantrone, procarbazine, trabectedin, clofarabine, amsacrine, brostalicin, pixantrone, laromustine; bleomycin, dactinomycin, doxorubicin, epirubicin, idarubicin, levamisole, miltefosine, mitomycin C, romidepsin, streptozocin, valrubicin, zinostatin, zorubicin, daunurobicin, plicamycin, aclarubicin, peplomycin, pirarubicin.